Fragment-based development of triazole-substituted O-galactosyl aldoximes with fragment-induced affinity and selectivity for galectin-3.
Author
Summary, in English
A fragment-based development of 3C-triazol-1-yl-O-galactopyranosyl aldoximes led to the discovery of highly selective and high affinity (K(d) down to 11 microm) small monosaccharide based inhibitors of galectin-3. Galectin-7, 8 N-terminal CRD, and 9 N-terminal CRD bound the inhibitors only weakly. The galectin-3 selectivity was hypothesized to stem from interaction of the aldoxime moiety with a site not present in the other galectins.
Department/s
Publishing year
2009
Language
English
Pages
3982-3990
Publication/Series
Organic and Biomolecular Chemistry
Volume
7
Issue
19
Document type
Journal article
Publisher
Royal Society of Chemistry
Topic
- Immunology in the medical area
- Microbiology in the medical area
Status
Published
ISBN/ISSN/Other
- ISSN: 1477-0539